|Oxytocin Chemical Properties|
|Oxytocin Usage And Synthesis|
|Uterine contraction drugs||Oxytocin is also called Pitocin, is a kind of uterine contraction medicine, can be extracted from animal posterior pituitary or chemical synthesis, chemical synthesis including on vasopressin, no booster effect, selective excitate uterine smooth muscle, strengthen its contracting, uterus is most sensitive to oxytocin (estrogen secretion increase) when parturient , immature uterus have no reactivity to this product, pregnancy early or middle uterine have low reactivity to oxytocin, late pregnancy is gradually increased, and before the antepartum, the reactivity is the highest. Small dose can strengthen the smooth muscle contraction rhythm at the bottom of the uterine, to reinforce the contraction force, contraction frequency, shrinkage properties similar to those in natural birth, and keep the polarity and symmetry, so the clinical used in hastening parturition, inducing abortion. Large dose make uterine muscle tetanic contraction, clinical to oppression blood vessels between muscle fibers, to prevent and treatment of postpartum hemorrhage and postpartum subinvolution, and has the effect to promote lactation, the breast duct contraction, prompting milk from the breast, but cannot increase milk secretion, only can promote the milk. It is important to strictly master the dose and dripping speed for hastening parturition or inducing abortion, lest cause tetanic uterine contractions, killing fetal distress or uterine rupture. Every cephalopelvic disproportion , malposition or other abnormality, it is forbidden , abnormal uterine contraction, has a history of cesarean section and 3 or more times a multipara is forbidden . The extraction of oxytocin from cows, pigs’ pituitaries accidentally cause allergic reaction, the too fast of static drop can cause mild vasodilation, blood pressure drops. The fastest speed is not more than 40 ~ 60 drops per minute. Larger dose is also used in postpartum hemorrhage, the afterbirth not out, etc. In recent years, it is found that this product has good effect on pulmonary hemoptysis, and vagus nerve after resection or relaxation of gastrointestinal function after abdominal surgery.
Oral invalid, easily destroyed by digestive juice, but can be oral cavity mucous membrane absorption, intravenous drip 0.01 IU can cause uterine physiological contraction in 1 ~ 3 minutes (rhythmicity, polarity, symmetry), hold time is short, the half-life is only 2.5 ~ 3 minutes high-dose make uterine muscle is tetanic contraction. Have synergy effect with prostaglandin.|
Common used with ergot preparations, treatment for postpartum hemorrhage; Inevitable abortion; Mainly used in late pregnancy induced labor and intrapartum uterine contractions fatigue caused by prolonged labor; Used for oxytocin sensitive test; Used for oxytocin irritability test; Assist in postpartum milk discharge; Haemoptysis. Postoperative gastrointestinal peristalsis slowly.
The above information is edited by the Chemicalbook of Duan Yalan.
|Chemical Properties||White to brown powder, has the water absorbability, soluble in water.|
|Application||This product can absorb from the oral mucosa, and selectively acts on the smooth muscle of the uterus, make uterine contractions. Apply to hastening parturition and slow painful. Effect is the same as the static drops of oxytocin. For contracted pelvis, has a history of uterine surgery (including cesarean section), pain excessive hyperfunction, birth canal obstruction, severe placental abruption, maternal pregnancy poisoning are prohibited. |
Uterine contractions. Used for induced labor, oxytocin, postpartum and abortion after uterine bleeding caused by contractions weak and so on. Intranasal can make milk.
Adverse reactions and taboos: birth, apparent cephalopelvic disproportion , completeness, placenta previa, umbilical cord presentation or prolapse, pelvic too narrow and too contractions are forbade. Placental abruption, heart disease, the uterus is too large, pregnant women over 35 years old, has a history of cesarean section, uterine fibroids rejecting history and breech is produced with caution. Sacral canal blocking with oxytocin, can happen serious hypertension, cerebrovascular even rupture. Cannot solution injection together with norepinephrine. Taboo compatibility with protein hydrolysate.
|Production Method||Method 1, extraction method (using in China, the purity is low, but the cost is low) |
Oxytocin liquid extract.
Take 100 g of leaf powder, 30 g of quartz powder in the ball mill, add distilled water, extracting four times with the same method. Join 1.4 L of distilled water two times, 1.3 L twice. Each extract 45 min, centrifugal, collect the liquid and residue is extracted. Merge extract of the four times for a quick fluid of oxytocin.
After leaf powder/water, ball mill →oxytocin extract.
Add 1500 g of good handled synthetic zeolite to 20 L of 0.25% acetic acid solution, stir and pour exchange column with ethyl acid decreased by more than to the surface of zeolite 2-3 cm, add to extract liquor , collect white turbid fluid (mainly contains oxytocin, because of its pI is 7.7, and vasopressin pI is 10.9, easy to become positively charged ions by adsorption) under appropriate velocity. When the extract liquid level down to the surface of zeolite, immediately join the distilled water, continue to collect turbid liquid until the flow. Turbid liquid with glacial acetic acid the pH of 3.5, in the water bath quickly heated to 95 oC, keep 3 min, rapid cooling and refrigerate overnight.
Oxytocin extract [HAc, synthetic zeolite]→turbid liquid [HAc, heating]→ separation liquid.
Adsorption, elution to the next day, filtrate the refrigerated liquid, add 10% bentonite slurry (per 100 ml and 3 ml) to the filtrate under stirring, stir 1 h, adsorption, centrifugation. Examinate Supernatant fluid with sulfosalicylic acid fluid, not settling for adsorption completely. If not completely, adsorption again, merging two bentonite slurry precipitation. Bentonite elution four times with 1% acetic acid (1.6 L and 1.4 L and 1.2 L and 0.8 L), every time add the eluent with tertiary butyl alcohol when heated to 80 oC, then heat up to 95 oC, rapid cooling to 25 oC, filtration or centrifuge, merge the filtrate, four testing titer and vasopressin.
Refrigerated liquid [filter] →filtrate liquor [bentonite slurry]→ adsorbate [ 1% HAc]→ eluent
Oxytocin injection preparation
Dilute qualified oxytocin liquid to 5u/ml or 10 u/ml, through 4 or 5 sintered filter funnel, potting, circulating steam sterilization for 30 min at 100 oC to obtain product.
Oxytocin liquid (measurement qualified) [filter filling and sealing]→oxytocin injection.
Note: synthetic zeolite treatment
New zeolite after 60-80 mesh sieve, added 2 L distilled water per 500 g, use sodium hydroxide to adjust to pH9, keep half an hour, leaning to the supernatant, add 2 L water, adjust pH to 9 again, pour to clear liquid again, add water, stir and add dilute sulphuric acid to pH 5.8-6 and stir for half an hour, pour to clear liquid, wash 7-8 times repeatedly and each time with water. Add1 L water and dilute sulphuric acid, mixed for half an hour, pour to clear liquid, washed with water to pH7, drain and dry. Set aside.
Regeneration of synthetic zeolite
Wash synthetic zeolite twice times with distilled water, then add 1.5 L of water (calculated on zeolite 500 g) and 150 g of sodium chloride, stir for 2 h, wash to remove vasopressin, again wash with distilled water to without chloride ion. Add right amount water, with sodium hydroxide to adjust pH to 9, mix half an hour, pour to clear liquid, wash with distilled water, with sulfuric acid to adjust pH to 5.5-6, and then washed with water to nearly neutral, drain, dried at 105 oC. Set aside. Before using, add right amount of water and glacial acetic acid, stirring soak.
10% of Bentonite slurry preparation
mixed bentonite with water according to the volume proportion of 1:10, grinding about 1 h, and adjust the grinding with acetic acid to pH 3.5, placed in the refrigerator and set aside.
Method 2, chemical synthesis method
Start with benzyl oxygen carbonyl leucine p-nitrophenyl acetate synthesis peptide 7 amide (3-9), synthesis of benzyl oxygen carbonyl acyl - S - benzyl in, cheese ammonia acyl azide (1-2 paragraphs), the third step synthetic oxytocin.
|Chemical Properties||White Solid|
|Usage||Oxytocin is the principal uterus-contracting and lactation-stimulating hormone of the posterior pituitary gland.|
|Oxytocin Preparation Products And Raw materials|